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| Other Sizes |
| Targets |
Ethacridine lactate exerts its primary antimicrobial effect by intercalating into bacterial DNA. This interaction disrupts critical cellular processes, ultimately leading to bacteriostasis. The compound binds to DNA, inhibiting the ability of bacteria to synthesize DNA and RNA, thereby inhibiting microbial protein synthesis. It is effective against Staphylococcus aureus, including MRSA strains.
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| ln Vitro |
Acrinol exhibits antimicrobial activity against Staphylococcus aureus, including MRSA, with a MIC range of 100-200 μg/mL. The minimum inhibitory concentration (MIC) of Acrinol for E. Coli is 200–800 μg/mL, while the MIC surpasses 1,600 μg/mL for Proteus vulgaris and Proteus mirabilis[3].
Ethacridine lactate demonstrates antimicrobial activity against Staphylococcus aureus and other Gram-positive cocci. The minimum inhibitory concentration (MIC) against Staphylococcus aureus, including MRSA, ranges from 100-200 μg/mL. Against E. coli, the MIC ranges from 200-800 μg/mL. It also functions as a PARG inhibitor, a property that is utilized in research applications. |
| ln Vivo |
Pregnancy can be ended with ethacridine lactate [1].
Ethacridine lactate is used in vivo as an antiseptic and abortifacient. As a topical antiseptic, it is applied to wounds and skin infections to prevent or treat bacterial infections. As an abortifacient, it is used for the induction of mid-trimester abortions. Its efficacy is based on its antimicrobial activity and its ability to stimulate uterine contractions. |
| Enzyme Assay |
Non-cellular assays for ethacridine lactate involve assessing its DNA intercalation properties. The compound's binding to DNA can be studied using spectrophotometric methods, such as measuring changes in the absorption spectrum of the compound upon addition of DNA. PARG inhibition can be assessed using purified PARG enzyme in a cell-free system, where the hydrolysis of poly(ADP-ribose) is measured in the presence of varying concentrations of the compound.
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| Cell Assay |
In vitro cellular assays for ethacridine lactate involve treating bacterial cultures with the compound and assessing growth inhibition. The minimum inhibitory concentration (MIC) is determined by broth microdilution according to CLSI guidelines. For PARG inhibition studies, cells are treated with the compound and PAR (poly(ADP-ribose) levels are measured by Western blotting or immunofluorescence to assess the inhibition of PAR degradation.
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| Animal Protocol |
In vivo animal experiments with ethacridine lactate are primarily conducted for toxicological assessment rather than efficacy studies, as it is a well-established drug. In preclinical models, it would be administered via appropriate routes (topical, intra-amniotic) to evaluate its safety and potential side effects. For research on its PARG inhibitory activity, animal models of disease where PARG plays a role may be used.
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| ADME/Pharmacokinetics |
Ethacridine lactate monohydrate has a molecular weight of 361.35 and a molecular formula of C₁₅H₁₅N₃O·C₃H₆O₃·H₂O. It is a yellow crystalline powder with a purity of ≥98%. The compound is soluble in water and is typically stored at room temperature in a dry, dark place. It is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Ethacridine lactate is generally well-tolerated when used topically as an antiseptic. Systemic toxicity is low due to limited absorption. However, as with any drug, allergic reactions may occur. When used as an abortifacient, it can cause uterine bleeding and other complications. Standard safety precautions should be followed when handling the compound.
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| References |
[1]. Gupta S, et, al. Ethacridine lactate -- a safe and effective drug for termination of pregnancy. Indian J Matern Child Health. 1993;4(2):59-61.
[2]. Rotin LE, et al. Erlotinib synergizes with the poly(ADP-ribose) glycohydrolase inhibitor ethacridine in acute myeloid leukemia cells. Haematologica. 2016 Nov;101(11):e449-e453. [3]. Usuki R, et, al. Antibacterial Activity of Acrinol against Organisms Isolated from Clinical Materials and Influence of Light on Antibacterial Activity of Acrinol. Japanese Journal of Pharmaceutical Health Care and Sciences. 2004 Jan; 30(2):72-77. |
| Additional Infomation |
Topical anti-infective agents.
Ethacridine lactate monohydrate (Acrinol; CAS 6402-23-9) is a versatile compound with antiseptic and PARG inhibitory activities. Its primary antimicrobial mechanism involves DNA intercalation, and it is effective against Gram-positive bacteria including MRSA. It is widely used as a topical antiseptic and as an abortifacient, and also serves as a research tool for studying PARG function and poly(ADP-ribose) metabolism. |
| Molecular Formula |
C18H23N3O5
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|---|---|
| Molecular Weight |
361.398
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| Exact Mass |
361.163
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| CAS # |
6402-23-9
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| Related CAS # |
Ethacridine lactate;1837-57-6
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| PubChem CID |
165457
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
523.5ºC at 760 mmHg
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| Melting Point |
243-245 °C(lit.)
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| Flash Point |
270.4ºC
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| LogP |
3.501
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
371
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C([H])([H])C([H])([H])[H])C1C([H])=C([H])C2C(C=1[H])=C(C1C([H])=C([H])C(=C([H])C=1N=2)N([H])[H])N([H])[H].O([H])C([H])(C(=O)O[H])C([H])([H])[H].O([H])[H]
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| InChi Key |
NYEPHMYJRNWPLA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H15N3O.C3H6O3.H2O/c1-2-19-10-4-6-13-12(8-10)15(17)11-5-3-9(16)7-14(11)18-13;1-2(4)3(5)6;/h3-8H,2,16H2,1H3,(H2,17,18);2,4H,1H3,(H,5,6);1H2
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| Chemical Name |
7-ethoxyacridine-3,9-diamine;2-hydroxypropanoic acid;hydrate
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| Synonyms |
Ethodin; Rivanol monohydrate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~276.71 mM)
H2O : ~2 mg/mL (~5.53 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.92 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7670 mL | 13.8351 mL | 27.6702 mL | |
| 5 mM | 0.5534 mL | 2.7670 mL | 5.5340 mL | |
| 10 mM | 0.2767 mL | 1.3835 mL | 2.7670 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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